EP 652 009 A1 describes inhibitors of aspartate protease which inhibit the production of beta-amyloid peptides in cell culture and in vivo.
WO 00/69262 discloses a beta-secretase and the use thereof in assays for finding potential active substances for the treatment of AD.
WO 01/00663 discloses memapsin 2 (human beta-secretase) as well as a recombinant catalytically active enzyme. Methods of identifying inhibitors of memapsin 2 are also described.
WO 01/00665 discloses inhibitors of memapsin 2 for the treatment of AD.
WO 03/057721 discloses substituted aminocarboxamides for the treatment of AD.
WO 05/004802 discloses substituted benzyl substituted N-alkyl-phenylcarboxamides for the treatment of AD.
The International patent applications WO 06/024932, WO 06/017836 and WO 06/017844 disclose substituted amino-quinazolines and their use as β-secretase inhibitors for the treatment of Alzheimer's disease.
At present there are no effective treatment methods capable of preventing, stopping or reversing AD.
Surprisingly, it has been found that the compounds of the present invention inhibit beta secretase-mediated cleavage of APP, are weakly basic, are only partially protonated at physiological conditions, show a high ability to overcome the blood/brain barrier and show improved selectivity against a variety of other biological targets.